禹州漏芦均一多糖的结构分析及其硫酸化衍生物的抗补体活性  

Structural Characterization of One Homogeneous Polysaccharide from Echinops latifolius Tausch. and Anti-complementary Activity of Its Sulfated Derivatives

作　　者：鲍斌[1] 王辉俊[1] 王宏伟[1] 施松善[1] 王顺春[1] 

机构地区：[1]上海中医药大学中药研究所中药标准化教育部重点实验室中药新资源与质量标准综合评价国家中医药管理局重点研究室,上海201203

出　　处：《高等学校化学学报》2014年第10期2119-2123,共5页Chemical Journal of Chinese Universities

基　　金：国家自然科学基金(批准号:81373951);重大新药创制专项(批准号:2012ZX09301001-003)资助~~

摘　　要：以禹州漏芦为原料,经沸水提取、乙醇沉淀、DEAE-Cellulose和SuperdexTM75凝胶柱层析分离纯化,得到一种水溶性的酸性均一多糖(EPS-2A).采用单糖组成、甲基化及绝对构型等方法对其进行了结构解析.结果表明,该均一多糖主要由D-半乳糖醛酸组成,并含有少量的Rha和Ara.该均一多糖经不同条件硫酸衍生化后的衍生物(Sul-2A-1和Sul-2A-2)与阳性药肝素[CH50=(103.0±9.0)μg/mL(mean±SD,n=3),CH50为出现50%溶血时的样品浓度]相比,均表现出很强的抗补体活性[Sul-2A-1的CH50=(74.1±4.6)μg/mL;Sul-2A-2的CH50=(35.7±2.8)μg/mL].To isolate and characterize the anti-complementary polysaccharide from the root of Echinops latifolius Tausch. , bioactivity-guided fractionation and purification was used to obtain the anti-complementary polysaccharide from the hot-water extract of the root of Echinops latifolius Tausch. The polysaccharide was characterized by various chemical and spectral analyses The anti-complementary activities were evaluated by hemolytic assay in vitro. The action targets were identified in the system with individual complement-depleted sera. A homogenous water-soluble polysaccharide （EPS-2A） was obtained from Echinops latifolius Tausch. , which average molecular weight was estimated to be 118000. A combination of monosaccharide composition, methylation and configuration analysis, as well as NMR spectroscopy, indicated that EPS-2A was poly-（ 1-4）- a-D-galactopyranosyluronic acid in which （87.8 ±0. 5 ）% of uronic acid existed as methylester. Two sulfated derivatives（ Sul-2A-1 and Sul-2A-2 ） from EPS-2A were prepared after sulfation with 1 ： 1 and 2 ： 1 of chlorosulfonic acid and pyridine, respectively. The anti-complementary assay showed that Sul-2A-1 and Sul-2A-2 demonstrated a stronger inhibitory effect [ CHs0 = （74. 1±4.6） μg/mL for Sul-2A-1 ; CH50 = （35.7±2. 8） μg/mL for Sul-2A-2] on the complement activation through the classic pathway, compared to that of heparin [ CHso = （103.0±9.0） μg/mL]. The results suggested that the sulfated derivatives Sul-2A-1 and Sul-2A-2 might be promising drug candidates in case of necessary therapeutic complement inhibition.

关 键 词：禹州漏芦 多糖 结构分析 硫酸衍生化 抗补体 

分 类 号：O629.12[理学—有机化学]